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Compound Detail

CHEMBL4754002

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COc1cccc(-n2cc(COc3cccc4cnc(Nc5cccc(Cl)c5)nc34)nn2)c1

Basic Information

ChEMBL ID CHEMBL4754002
Phase Preclinical
Structure Type MOL
InChI Key MFQCHZGEEFBQCA-UHFFFAOYSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

458.9
MW (Da)
5.20
ALogP
8
HBA
1
HBD
87.0
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H19ClN6O2
MW 458.91
Aromatic Rings 5
Heavy Atoms 33
NP-Likeness -1.94

Activity Summary

IC50 7 meas. best 5.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
IC50 5.1 5.1 8000.0 1
PC-3
CHEMBL390
IC50 5.0 5.0 10000.0 1
Fibroblast
CHEMBL5314315
IC50 4.75 4.75 18000.0 1
Caco-2
CHEMBL614058
IC50 4.7 4.7 20000.0 1
HCT-116
CHEMBL394
IC50 4.64 4.64 23000.0 1
Huh-7
CHEMBL614039
IC50 4.64 4.64 23000.0 1
MDA-MB-231
CHEMBL400
IC50 4.6 4.6 25000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33422908 10.1016/j.bmc.2020.115962 Cyclin-dependent kinase 5/CDK5 activator 1 1
33422908 10.1016/j.bmc.2020.115962 CDK9/cyclin T1 1
33422908 10.1016/j.bmc.2020.115962 Serine/threonine-protein kinase pim-1 1
33422908 10.1016/j.bmc.2020.115962 Dual specificity protein kinase CLK1 1
33422908 10.1016/j.bmc.2020.115962 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
33422908 10.1016/j.bmc.2020.115962 Serine/threonine-protein kinase haspin 1
33422908 10.1016/j.bmc.2020.115962 Glycogen synthase kinase-3 beta 1
33422908 10.1016/j.bmc.2020.115962 Casein kinase I isoform epsilon 1
33422908 10.1016/j.bmc.2020.115962 Huh-7 1
33422908 10.1016/j.bmc.2020.115962 Caco-2 1
33422908 10.1016/j.bmc.2020.115962 MDA-MB-231 1
33422908 10.1016/j.bmc.2020.115962 HCT-116 1
33422908 10.1016/j.bmc.2020.115962 PC-3 1
33422908 10.1016/j.bmc.2020.115962 NCI-H727 1
33422908 10.1016/j.bmc.2020.115962 MCF7 1
33422908 10.1016/j.bmc.2020.115962 Fibroblast 1

Data from ChEMBL 36 via Core Engine